A novel reactivity of organoboronic acids with bicyclic hydrazines leading to the stereoselective formation of trans-vicinal disubstituted cyclopentenes in good to excellent yield is discussed. The reaction of cyclopentadiene and fulvene derived azabicyclic alkenes with organoboronic acids afforded the trans-3,4-disubstituted cyclopentenes and alkylidene cyclopentenes in good to excellent yields. The products, having a broad range of substituents, are important intermediates in the synthesis of a number of pharmaceutically important molecules.
讨论了有机
硼酸与双环
肼的一种新的反应性,该反应性导致立体选择性地形成跨邻位双取代
环戊烯,并且产率良好至优异。
环戊二烯和富烯衍生的
氮杂双环烯烃与有机
硼酸的反应以良好至优异的产率提供反式3,4-二取代
环戊烯和亚烷基
环戊烯。该产品具有广泛的取代基,是合成许多药学上重要分子的重要中间体。